Novel methodology to identify TRPV1 antagonists independent of capsaicin activation (Q39498595)

12 September 2017

Novel methodology to identify TRPV1 antagonists independent of capsaicin activation (English)

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12 September 2017

Stephen Zicha

1

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12 September 2017

Olivier Radresa

2

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12 September 2017

Patricia Laplante

3

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12 September 2017

Michael Morton

4

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12 September 2017

Karen Jones

5

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12 September 2017

Martin Main

6

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12 September 2017

Shephali Trivedi

7

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12 September 2017

Ron P Julien

8

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12 September 2017

Andrew Griffin

9

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12 September 2017

Jean Labrecque

10

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12 September 2017

Sultan Ahmad

11

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12 September 2017

William Brown

12

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12 September 2017

20 December 2012

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Journal of Biomolecular Screening

12 September 2017

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12 September 2017

18

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12 September 2017

5

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12 September 2017

544-555

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Impaired nociception and pain sensation in mice lacking the capsaicin receptor

12 September 2017

1 reference

https://api.crossref.org/works/10.1177%2F1087057112470563

Clinical development of TRPV1 antagonists: targeting a pivotal point in the pain pathway

21 January 2018

1 reference

https://api.crossref.org/works/10.1177%2F1087057112470563

The capsaicin receptor: a heat-activated ion channel in the pain pathway

21 January 2018

1 reference

https://api.crossref.org/works/10.1177%2F1087057112470563

Therapeutic potential of vanilloid receptor TRPV1 agonists and antagonists as analgesics: Recent advances and setbacks

21 January 2018

1 reference

https://api.crossref.org/works/10.1177%2F1087057112470563

Body-temperature maintenance as the predominant function of the vanilloid receptor TRPV1

21 January 2018

1 reference

https://api.crossref.org/works/10.1177%2F1087057112470563

Transient receptor potential vanilloid-1 antagonists: a survey of recent patent literature

21 January 2018

1 reference

https://api.crossref.org/works/10.1177%2F1087057112470563

N-(4-Tertiarybutylphenyl)-4-(3-chloropyridin-2-yl)tetrahydropyrazine -1(2H)-carbox-amide (BCTC), a Novel, Orally Effective Vanilloid Receptor 1 Antagonist with Analgesic Properties: I. In Vitro Characterization and Pharmacokinetic Properties

21 January 2018

1 reference

https://api.crossref.org/works/10.1177%2F1087057112470563

Identification and characterisation of SB-366791, a potent and selective vanilloid receptor (VR1/TRPV1) antagonist.

21 January 2018

1 reference

https://api.crossref.org/works/10.1177%2F1087057112470563

AMG 9810 [(E)-3-(4-t-butylphenyl)-N-(2,3-dihydrobenzo[b][1,4] dioxin-6-yl)acrylamide], a novel vanilloid receptor 1 (TRPV1) antagonist with antihyperalgesic properties

21 January 2018

1 reference

https://api.crossref.org/works/10.1177%2F1087057112470563

Identification of (R)-1-(5-tert-butyl-2,3-dihydro-1H-inden-1-yl)-3-(1H-indazol-4-yl)urea (ABT-102) as a potent TRPV1 antagonist for pain management

21 January 2018

1 reference

https://api.crossref.org/works/10.1177%2F1087057112470563

Novel vanilloid receptor-1 antagonists: 2. Structure-activity relationships of 4-oxopyrimidines leading to the selection of a clinical candidate

21 January 2018

1 reference

https://api.crossref.org/works/10.1177%2F1087057112470563

Characterization of SB-705498, a potent and selective vanilloid receptor-1 (VR1/TRPV1) antagonist that inhibits the capsaicin-, acid-, and heat-mediated activation of the receptor

21 January 2018

1 reference

https://api.crossref.org/works/10.1177%2F1087057112470563

Gating of TRP channels: a voltage connection?

21 January 2018

1 reference

https://api.crossref.org/works/10.1177%2F1087057112470563

Sodium channel inhibitor drug discovery using automated high throughput electrophysiology platforms

21 January 2018

1 reference

https://api.crossref.org/works/10.1177%2F1087057112470563

Population patch clamp improves data consistency and success rates in the measurement of ionic currents

21 January 2018

1 reference

https://api.crossref.org/works/10.1177%2F1087057112470563

Automated voltage-clamp technique.

21 January 2018

1 reference

https://api.crossref.org/works/10.1177%2F1087057112470563

Optimisation and validation of a medium-throughput electrophysiology-based hNav1.5 assay using IonWorks.

21 January 2018

1 reference

https://api.crossref.org/works/10.1177%2F1087057112470563

QPatch: the missing link between HTS and ion channel drug discovery.

21 January 2018

1 reference

https://api.crossref.org/works/10.1177%2F1087057112470563

Ionworks HT: a new high-throughput electrophysiology measurement platform.

21 January 2018

1 reference

https://api.crossref.org/works/10.1177%2F1087057112470563

Cellular HTS assays for pharmacological characterization of Na(V)1.7 modulators

21 January 2018

1 reference

https://api.crossref.org/works/10.1177%2F1087057112470563

Mutation of Asn111 in the third transmembrane domain of the AT1A angiotensin II receptor induces its constitutive activation.

21 January 2018

1 reference

https://api.crossref.org/works/10.1177%2F1087057112470563

The vanilloid receptor TRPV1 is tonically activated in vivo and involved in body temperature regulation

21 January 2018

1 reference

https://api.crossref.org/works/10.1177%2F1087057112470563

Pharmacological characterization of the TRPV1 receptor antagonist JYL1421 (SC0030) in vitro and in vivo in the rat.

21 January 2018

1 reference

https://api.crossref.org/works/10.1177%2F1087057112470563

High affinity antagonists of the vanilloid receptor

21 January 2018

1 reference

https://api.crossref.org/works/10.1177%2F1087057112470563

Experimental and computational approaches to estimate solubility and permeability in drug discovery and development settings

21 January 2018

1 reference

https://api.crossref.org/works/10.1177%2F1087057112470563

Ca2+/calmodulin modulates TRPV1 activation by capsaicin.

21 January 2018

1 reference

https://api.crossref.org/works/10.1177%2F1087057112470563

Transient receptor potential channel A1 is directly gated by calcium ions

21 January 2018

1 reference

https://api.crossref.org/works/10.1177%2F1087057112470563

Antihyperalgesic effects of (R,E)-N-(2-hydroxy-2,3-dihydro-1H-inden-4-yl)-3-(2-(piperidin-1-yl)-4-(trifluoromethyl)phenyl)-acrylamide (AMG8562), a novel transient receptor potential vanilloid type 1 modulator that does not cause hyperthermia in rats

21 January 2018

1 reference

https://api.crossref.org/works/10.1177%2F1087057112470563

The principle of temperature-dependent gating in cold- and heat-sensitive TRP channels

21 January 2018

1 reference

https://api.crossref.org/works/10.1177%2F1087057112470563

Voltage is a partial activator of rat thermosensitive TRP channels

21 January 2018

1 reference

https://api.crossref.org/works/10.1177%2F1087057112470563

The biophysical and molecular basis of TRPV1 proton gating

21 January 2018

1 reference

https://api.crossref.org/works/10.1177%2F1087057112470563

Identification of molecular determinants of channel gating in the transient receptor potential box of vanilloid receptor I.

21 January 2018

1 reference

https://api.crossref.org/works/10.1177%2F1087057112470563

Pharmacological blockade of the vanilloid receptor TRPV1 elicits marked hyperthermia in humans

21 January 2018

1 reference

https://api.crossref.org/works/10.1177%2F1087057112470563

21 January 2018

Identifiers

DOI

10.1177/1087057112470563

1 reference

12 September 2017

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